One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins

DOI: 10.4236/pp.2013.48083   PDF   HTML     4,245 Downloads   6,392 Views   Citations

Abstract

An initial burst is often observed during the release of active pharmaceutical ingredients (APIs) from poly-lactic-coglycolic-acid (PLGA) microparticles (MPs) which have been prepared by the emulsion-solvent evaporation method. Herein, we describe the development of a simple one-step coating method that suppresses the initial burst release process. This new method involves coating the PLGA-MPs with PLGA, with the coating process being performed through the phase separation of PLGA on the surface of PLGA-MPs using the emulsion-solvent evaporation method. Bovine serum albumin (BSA) was encapsulated in the PLGA-MPs as a model API. The coated MPs were spherical in shape with no pores on their smooth surface, whereas the non-coated PLGA-MPs had porous surfaces. An in vitro release study showed that the residual levels of BSA in the coated and non-coated PLGA-MPs after 1 h were about 99% and 16% of the original loads, respectively. The one-step coating method therefore represents a useful method for preparing PLGA-MPs that do not give an initial burst release of proteinaceous APIs.

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H. Takabe, M. Ohkuma, Y. Iwao, S. Noguchi and S. Itai, "One-Step Preparation of Poly-Lactic-Co-Glycolic-Acid Microparticles to Prevent the Initial Burst Release of Encapsulated Water-Soluble Proteins," Pharmacology & Pharmacy, Vol. 4 No. 8, 2013, pp. 578-583. doi: 10.4236/pp.2013.48083.

Conflicts of Interest

The authors declare no conflicts of interest.

References

[1] R. A. Jain, “The Manufacturing Techniques of Various Drug Loaded Biodegradable Poly(Lactide-Co-Glycolide) (PLGA) Devices,” Biomaterials, Vol. 21, No. 23, 2000, pp. 2475-2490.
http://dx.doi.org/10.1016/S0142-9612(00)00115-0
[2] P. I. P. Park, M. Makoid and S. Jonnalagadda, “The Design of Flexible Ciprofloxacin-Loaded PLGA Implants Using a Reversed Phase Separation/Coacervation Method,” European Journal of Pharmaceutics and Biopharmaceutics, Vol. 77, No. 2, 2011, pp. 233-239.
http://dx.doi.org/10.1016/j.ejpb.2010.11.014
[3] K. Andreas, R. Zehbe, M. Kazubek, K. Grzeschik, N. Sternberg, H. Baumler, H. Schubert, M. Sittinger and J. Ringe, “Biodegradable Insulin-Loaded PLGA Microspheres Fabricated by Three Different Emulsification Techniques: Investigation for Cartilage Tissue Engineering,” Acta Biomaterialia, Vol. 7, No. 4, 2011, pp. 1485-1495.
http://dx.doi.org/10.1016/j.actbio.2010.12.014
[4] C. B. Weldon, J. H. Tsui, S. A. Shankarappa, V. T. Nguyen, M. Ma, D. G. Anderson and D. S. Kohane, “Electrospun Drug-Eluting Sutures for Local Anesthesia,” Journal of Controlled Release, Vol. 161, No. 3, 2012, pp. 903-909. http://dx.doi.org/10.1016/j.jconrel.2012.05.021
[5] T. Niwa, H. Takeuchi, T. Hino, M. Nohara and Y. Kawashima, “Biodegradable Submicron Carriers for Peptide Drugs: Preparation of dl-Lactide/Glycolide Copolymer (PLGA) Nanospheres with Nafarelin Acetate by a Novel Emulsion-Phase Separation Method in an Oil System,” International Journal of Pharmaceutics, Vol. 121, No. 1, 1995, pp. 45-54.
http://dx.doi.org/10.1016/0378-5173(95)00002-Z
[6] S. Mao, J. Xu, C. Cai, O. Germershaus, A. Schaper and T. Kissel, “Effect of WOW Process Parameters on Morphology and Burst Release of FITC-Dextran Loaded PLGA Microspheres,” International Journal of Pharmaceutics, Vol. 334, No. 1-2, 2007, pp. 137-148.
http://dx.doi.org/10.1016/j.ijpharm.2006.10.036
[7] Y. Yamaguchi, M. Takenaga, A. Kitagawa, Y. Ogawa, Y. Mizushima and R. Igarashi, “Insulin-Loaded Biodegradable PLGA Microcapsules: Initial Burst Release Controlled by Hydrophilic Additives,” Journal of Controlled Release, Vol. 81, No. 3, 2002, pp. 235-249.
http://dx.doi.org/10.1016/S0168-3659(02)00060-3
[8] C. Engineer, J. Parikh and A. Raval, “Effect of Copolymer Ratio on Hydrolytic Degradation of Poly (Lactideco-glycolide) from Drug Eluting Coronary Stents,” Chemical Engineering Research and Design, Vol. 89, No. 3, 2011, pp. 328-334.
http://dx.doi.org/10.1016/j.cherd.2010.06.013
[9] S. Xie, S. Wang, L. Zhu, F. Wang and W. Zhou, “The Effect of Glycolic Acid Monomer Ratio on the Emulsifying Activity of PLGA in Preparation of Protein-Loaded SLN,” Colloids and Surfaces B: Biointerfaces, Vol. 74, No. 1, 2009, pp. 358-361.
http://dx.doi.org/10.1016/j.colsurfb.2009.08.005
[10] B. S. Zolnik and D. J. Burgess, “Evaluation of in Vivo-in Vitro Release of Dexamethasone from PLGA Microspheres,” Journal of Controlled Release, Vol. 127, No. 2, 2008, pp. 137-145.
http://dx.doi.org/10.1016/j.jconrel.2008.01.004
[11] S. S. Chakravarthi and D. H. Robinson, “Enhanced Cellular Association of Paclitaxel Delivered in ChitosanPLGA Particles,” International Journal of Pharmaceutics, Vol. 409, No. 1-2, 2011, pp. 111-120.
http://dx.doi.org/10.1016/j.ijpharm.2011.02.034
[12] M. L. Manca, G. Loy, M. Zaru and A. M. Fadda, “Release of Rifampicin from Chitosan, PLGA and ChitosanCoated PLGA Microparticles,” Colloids and Surfaces B: Biointerfaces, Vol. 67, No. 2, 2008, pp. 166-170.
http://dx.doi.org/10.1016/j.colsurfb.2008.08.010
[13] H. Nojehdehian, F. Moztarzadeh, H. Baharvand, H. Nazarian and M. Tahriri, “Preparation and Surface Characterization of Poly-l-Lysine-Coated PLGA Microsphere Scaffolds Containing Retinoic Acid for Nerve Tissue Engineering: In Vitro Study,” Colloids and Surfaces B: Biointerfaces, Vol. 73, No. 1, 2009, pp. 23-29.
http://dx.doi.org/10.1016/j.colsurfb.2009.04.029
[14] J. Shen and D. J. Burgess, “Accelerated in Vitro Release Testing of Implantable PLGA Microsphere/PVA Hydrogel Composite Coatings,” International Journal of Pharmaceutics, Vol. 422, No. 1-2, 2012, pp. 341-348.
http://dx.doi.org/10.1016/j.ijpharm.2011.10.020
[15] A. Budhian, S. J. Siegel and K. I. Winey, “Controlling the in Vitro Release Profiles for a System of Haloperidol-Loaded PLGA Nanoparticles,” International Journal of Pharmaceutics, Vol. 346, No. 1-2, 2008, pp. 151-159.
http://dx.doi.org/10.1016/j.ijpharm.2007.06.011
[16] A. R. Ahmed, K. Elkharraz, M. Irfan and R. Bodmeier, “Reduction in Burst Release after Coating Poly(d,l-Lactide-Co-Glycolide) (PLGA) Microparticles with a DrugFree PLGA Layer,” Pharmaceutical Development and Technology, Vol. 17, No. 1, 2012, pp. 66-72.
http://dx.doi.org/10.3109/10837450.2010.513989
[17] A. R. Ahmed, A. Dashevsky and R. Bodmeier, “Reduction in Burst Release of PLGA Microparticles by Incorporation into Cubic Phase-Forming Systems,” European Journal of Pharmaceutics and Biopharmaceutics, Vol. 70, No. 3, 2008, pp. 765-769.
http://dx.doi.org/10.1016/j.ejpb.2008.07.008
[18] R. Jeyanthi, R. C. Mehta, B. C. Thanoo and P. P. Deluca, “Effect of Processing Parameters on the Properties of Peptide-Containing PLGA Microspheres,” Journal of Microencapsulation, Vol. 14, No. 2, 1997, pp. 163-174.
http://dx.doi.org/10.3109/02652049709015330
[19] H. K. Makadia and S. J. Siegel, “Poly Lactic-Co-Glycolic Acid (PLGA) as Biodegradable Controlled Drug Delivery Carrier,” Polymers, Vol. 3, No. 3, 2011, pp. 1377-1397.
http://dx.doi.org/10.3390/polym3031377
[20] G. Mittal, D. K. Sahana, V. Bhardwaj and M. N. V. Ravi Kumar, “Estradiol Loaded PLGA Nanoparticles for Oral Administration: Effect of Polymer Molecular Weight and Copolymer Composition on Release Behavior in Vitro and in Vivo,” Journal of Controlled Release, Vol. 119, No. 1, 2007, pp. 77-85.
http://dx.doi.org/10.1016/j.jconrel.2007.01.016

  
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